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> GI254023X [260264-93-5]

GI254023X [260264-93-5]

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Référence HY-19956-5mg

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GI254023X is a potent MMP9 and ADAM10 inhibitor with IC50s of 2.5 and 5.3 nM, respectively.

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GI254023X Chemical Structure

GI254023X Chemical Structure

CAS No. : 260264-93-5

This product is a controlled substance and not for sale in your territory.

Based on 10 publication(s) in Google Scholar

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Description

GI254023X is a potent MMP9 and ADAM10 inhibitor with IC50s of 2.5 and 5.3 nM, respectively.

IC50 & Target

IC50: 2.5 nM (MMP9), 5.3 nM (ADAM10)[1]
In Vitro

In cellular assay 25 μM and even a concentration of 1 μM GI254023X strongly reduces constitutive RAGE shedding; also PACAP-inducing shedding of RAGE is significantly reduced. At a concentration of 100 nM, a slight inhibition of RAGE shedding is still observed. In in vitro assays with recombinant proteinases, GI254023X discriminates between ADAM17 (IC50=541 nM) and ADAM10 (IC50=5.3 nM)/MMP9 (IC50=2.5 nM)[1]. CXCL16 shedding is inhibited by ADAM protease inhibitors (e.g GI254023x). A2780 cells are incubated with the ADAM-10/ADAM-17 inhibitor TAPI-2, as well as the ADAM-10-selective inhibitor GI254023x, as the level of expressed ADAM-10 is on average 9.8-fold higher on mRNA level compare with ADAM-17. In addition, GI254023x also prevents CXCL16 shedding from the cell membrane and is even more potent than TAPI-2[2]. When apply the specific ADAM10 (α-secretase) inhibitor GI254023X (5 mM) to serum/glucose-deprived slices, PI counts are significantly increased in comparison with DMSO (carrier)-treated controls[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GI254023X Related Antibodies
Masse moléculaire

391.50

Formule

C21H33N3O4
CAS No.

260264-93-5
Appearance

Solid

Color

White to off-white

SMILES

O=C(N[C@H](C(NC)=O)C(C)(C)C)[C@@H]([C@@H](N(C=O)O)C)CCCC1=CC=CC=C1
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvant et solubilité
In Vitro: 

DMSO : 100 mg/mL (255.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5543 mL 12.7714 mL 25.5428 mL
5 mM 0.5109 mL 2.5543 mL 5.1086 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Calculateur de molarité

  • Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation

Purity: 99.67%

COA (251 KB) LCMS (367 KB)

Instruction de manipulation (2659 KB)
Références

  • [1]. Verena V. Metz, et al. Induction of RAGE Shedding by Activation of G Protein-Coupled Receptors. PLoS One. 2012.  [Content Brief]

    [2]. M J M Gooden, et al. Elevated serum CXCL16 is an independent predictor of poor survival in ovarian cancer and may reflect pro-metastatic ADAM protease activity. British Journal of Cancer (2014) 110, 1535–1544.  [Content Brief]

    [3]. N Milosch, et al. Holo-APP and G-protein-mediated signaling are required for sAPPa-induced activation of the Akt. Cell Death Dis. 2014 Aug 28;5:e1391.  [Content Brief]

Test cellulaire
[3]

Cell death is quantified based on plasma membrane permeabilization. When apply the ADAM10 (a-secretase) inhibitor GI254023X (5 mM), slices are cultured in serum-/glucose-free medium for 48 h containing the inhibitor or its respective carrier (DMSO) as control. Round circles of identical size (Ø 500mm) are positioned in equivalent locations within the CA1 region of each hippocampus image and all PI-stained cells are counted using software. Cell viability assays are performed with a commercial kit according to the manufacturer’s instructions. The assay quantitates ATP levels, an indicator of metabolically active cells, photometrically with a fluorescence plate reader. Additionally, the live-dead cell staining kit are applied according to the manual. Cells are simultaneously stained with green fluorescent calcein-AM (4mM; ex/em: 495/515 nm) to detect intracellular esterase activity (viable cells) and red fluorescent ethidium homodimer-3 (2mM; ex/em: 530/635 nm) to indicate loss of plasma membrane integrity (dead cells)[3].

MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Références

  • [1]. Verena V. Metz, et al. Induction of RAGE Shedding by Activation of G Protein-Coupled Receptors. PLoS One. 2012.  [Content Brief]

    [2]. M J M Gooden, et al. Elevated serum CXCL16 is an independent predictor of poor survival in ovarian cancer and may reflect pro-metastatic ADAM protease activity. British Journal of Cancer (2014) 110, 1535–1544.  [Content Brief]

    [3]. N Milosch, et al. Holo-APP and G-protein-mediated signaling are required for sAPPa-induced activation of the Akt. Cell Death Dis. 2014 Aug 28;5:e1391.  [Content Brief]

  • [1]. Verena V. Metz, et al. Induction of RAGE Shedding by Activation of G Protein-Coupled Receptors. PLoS One. 2012.

    [2]. M J M Gooden, et al. Elevated serum CXCL16 is an independent predictor of poor survival in ovarian cancer and may reflect pro-metastatic ADAM protease activity. British Journal of Cancer (2014) 110, 1535–1544.

    [3]. N Milosch, et al. Holo-APP and G-protein-mediated signaling are required for sAPPa-induced activation of the Akt. Cell Death Dis. 2014 Aug 28;5:e1391.

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5543 mL 12.7714 mL 25.5428 mL 63.8570 mL
5 mM 0.5109 mL 2.5543 mL 5.1086 mL 12.7714 mL
10 mM 0.2554 mL 1.2771 mL 2.5543 mL 6.3857 mL
15 mM 0.1703 mL 0.8514 mL 1.7029 mL 4.2571 mL
20 mM 0.1277 mL 0.6386 mL 1.2771 mL 3.1928 mL
25 mM 0.1022 mL 0.5109 mL 1.0217 mL 2.5543 mL
30 mM 0.0851 mL 0.4257 mL 0.8514 mL 2.1286 mL
40 mM 0.0639 mL 0.3193 mL 0.6386 mL 1.5964 mL
50 mM 0.0511 mL 0.2554 mL 0.5109 mL 1.2771 mL
60 mM 0.0426 mL 0.2129 mL 0.4257 mL 1.0643 mL
80 mM 0.0319 mL 0.1596 mL 0.3193 mL 0.7982 mL
100 mM 0.0255 mL 0.1277 mL 0.2554 mL 0.6386 mL
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GI254023X Related Classifications

Help & FAQs

Keywords:

GI254023X260264-93-5GI4023 SRI028594GI 4023GI-4023SRI028594SRI 028594SRI-028594MMPMatrix metalloproteinasesInhibitorinhibitorinhibit

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